The present invention relates to a series of novel derivatives of the compound rhizoxin. The invention also provides a process for preparing such compounds and methods and compositions for using them.
Rhizoxin itself is a known substance having the following formula: ##STR1##
Rhizoxin itself and its acetate were disclosed in J. Antibiotics, 37, 354 (1984) and the anti-tumor activity of rhizoxin was disclosed in the Abstracts of the 43rd General Meeting of the Japanese Cancer Society, page 243, Title No. 1005 (1984).
Rhizoxin-2-ene was reported on Dec. 18th, 1984 to the 1984 International Chemical Congress of the Pacific Basin Society, Honolulu, Hawaii.
We have now discovered a series of rhizoxin derivatives which have far better anti-tumor activity than rhizoxin and its acetate and which have a lower toxicity than rhizoxin itself.